Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T7701 |
Boc-NH-PEG3
PROTAC Linker 10,2-[2-(2-T-BOC-氨基乙氧基)乙氧基]乙醇 |
Others; PROTAC Linker | Others; PROTAC |
Boc-NH-PEG3 (PROTAC Linker 10) 是一种属于 PEG 类的 PROTAC linker,可用于 PROTAC 的合成分子。 | |||
T14413 |
Azido-PEG10-alcohol
叠氮-十聚乙二醇 |
Others; PROTAC Linker | Others; PROTAC |
Azido-PEG10-alcohol 是一种属于 PEG 类的 PROTAC linker,可用于 PROTAC 分子的合成。 | |||
T17694 |
Br-C10-methyl ester
11-溴代十一烷酸甲酯 |
Others; PROTAC Linker | Others; PROTAC |
Br-C10-methyl ester 是一种属于 alkyl/ether 类的 PROTAC linker,可用于一系列 PROTAC 分子的合成。PROTAC 分子含有两个通过 linker 连接的不同配体,一种是 VHL 配体部分,另一种是靶蛋白配体。 | |||
T17881 |
(S,R,S)-AHPC-C10-NH2
VH032-C10-NH2 |
Others; Ligand for E3 Ligase | Others; PROTAC |
(S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) 包含基于 (S,R,S)-AHPC 的VHL 配体和 1 个 linker,是一种合成的 E3 连接酶配体-linker 偶联物 (E3 ligase ligand-linker conjugate)。用于 BET 的靶向 PROTAC 的合成。 | |||
T18661 |
(S,R,S)-AHPC-C10-NH2 dihydrochloride
VH032-C10-NH2 dihydrochloride,VH032-linker 10,(S,R,S)-AHPC-C10-NH2二盐酸盐,VH032 amide-alkylC10-amine |
Others; Ligand for E3 Ligase | Others; PROTAC |
(S,R,S)-AHPC-C10-NH2 dihydrochloride (VH032-linker 10) 包含基于 (S,R,S)-AHPC 的VHL 配体和 1 个 linker,是一种合成的 E3 连接酶配体-linker 偶联物,用于合成 BET 的靶向 PROTAC。 | |||
T18680 |
SD-36
|
Others; PROTACs | Others; PROTAC |
SD-36, a potent and efficacious PROTAC STAT3 degrader (Kd=~50 nM), exhibits high specificity for STAT3 over other STAT members. It effectively targets both wild-type and mutated STAT3 proteins in cells, inhibiting their transcriptional activity (IC50=10 nM). The compound, consisting of the STAT3 inhibitor SI-109, a linker, and a CRBN ligand Lenalidomide analog for E3 ubiquitin ligase[1], demonstrates significant anti-tumor effects and achieves complete, long-lasting tumor regression in mouse mod... | |||
T15120 |
Diethyl 10-bromodecylphosphonate
|
Others | Others |
Diethyl 10-bromodecylphosphonate is an alkyl-based PROTAC linker utilized for the synthesis of PROTACs[1]. | |||
T17901 |
cIAP1 Ligand-Linker Conjugates 10
E3 ligase Ligand-Linker Conjugates 47 |
Others | Others |
cIAP1 Ligand-Linker Conjugates 10 comprise of an IAP ligand and a PROTAC linker, which facilitates the design of SNIPERs. These conjugates incorporate an IAP ligand that interacts with the E3 ubiquitin ligase, and a PROTAC linker. SNIPERs can be developed using cIAP1 Ligand-Linker Conjugates 10. | |||
T13999 |
(10-BRomodecyl)phosphonic acid
|
Others | Others |
(10-BRomodecyl)phosphonic acid is an alkyl chain-derived PROTAC linker suitable for PROTAC synthesis [1]. | |||
T18515 |
Palbociclib-propargyl
PROTAC CDK6 ligand 1 |
Others | Others |
Palbociclib-propargyl, a PROTAC ligand targeting the protein CDK6, connects to the CRBN ligand through a PEG linker to form PROTAC CP-10. CP-10 exhibits a potent DC50 value of 2.1 nM against CDK6[1]. | |||
T14000 | [10-(Diethoxy-phosphoryl)-decyl]-phosphonic acid | Others | Others |
The compound [10-(diethoxy-phosphoryl)-decyl]-phosphonic acid is a suitable alkyl chain-based PROTAC linker for the synthesis of PROTACs [1]. | |||
T16583 |
Propargyl-PEG1-acid
|
Others | Others |
Propargyl-PEG1-acid, a PEG-based PROTAC linker, enables the synthesis of BTK-CRBN PROTACs, specifically Ibrutinib-based PROTAC 4 and PROTAC 5. At a concentration of 10 μM, PROTAC 5 facilitates the degradation of BTK and induces the degradation of CSK, LYN, and LAT2[1]. | |||
T17904 |
Pomalidomide-PEG1-C2-N3
E3 ligase Ligand-Linker Conjugates 50,Cereblon Ligand-Linker Conjugates 13 |
Others | Others |
Pomalidomide-PEG1-C2-N3 is a compound that has been synthesized as a conjugate of an E3 ligase ligand-linker. This compound incorporates the cereblon ligand based on Pomalidomide and a 1-unit PEG linker, which are commonly used in PROTAC technology. Utilizing Pomalidomide-PEG1-C2-N3, it is possible to design a selective CDK6 PROTAC degrader known as CP-10. CP-10 effectively induces the degradation of CDK6, displaying a DC50 value of 2.1 nM[1]. | |||
T18682 |
SJFδ
|
Others | Others |
SJFδ is a 10-atom linker PROTAC. SJFδ degrades p38δ with a DC50 of 46.17 nM, but does not degrade p38α, p38β, or p38γ[1]. | |||
T15834 |
m-PEG10-alcohol
Decaethylene glycol monomethyl ether |
Others | Others |
m-PEG10-alcohol, also known as Decaethylene glycol monomethyl ether, is a non-cleavable 10 unit PEG ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs)[1]. Additionally, m-PEG10-alcohol serves as a PEG-based PROTAC linker, enabling its application in the synthesis of PROTACs[1]. | |||
T71919 |
Boc-10-Aminodecanoic acid
|
||
Boc-10-Aminodecanoic acid can be used as a PROTAC linker in the synthesis of PROTACs and other conjugation applications. Boc-10-Aminodecanoic acid is an alkane chain with terminal carboxlic acid and Boc-protected amino groups. The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond. The Boc group can be deprotected under mild acidic conditions to form the free amine. | |||
T18601 |
Desmethyl-QCA276
PROTAC BRD4-binding moiety 4 |
Others | Others |
Desmethyl-QCA276, the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM[1]. | |||
T41146 |
ND1-YL2
ND1-YL2 |
||
ND1-YL2 is a peptide-based PROTAC®Degrader of steroid receptor co-activator 1 (SRC-1; also known as nuclear receptor coactivator 1, NCOA1). ND1-YL2 is composed of a stapled peptide that binds SRC-1 (YL2) joined by a linker to a tetrapeptide that binds UBR box domains. Upon ternary complex formation, SRC-1 is polyubiquitinated and subsequently degraded via the N-degron pathway. This Degrader induces dose-dependent degradation of SRC-1 in the MDA-MB-231 triple negative breast cancer cell line (DC5... | |||
T83856 |
AP-1
|
||
AP-1是一种微型化的蛋白质水解靶向嵌合体(PROTAC),由吲哚美辛(±)连接的间变性淋巴瘤激酶(ALK)配体和E3泛素连接酶配体通过超短连接器相连。在10至300 nM浓度范围内使用时,AP-1能高效降解Karpas-299细胞中高表达的ALK融合蛋白NPM-ALK,此效应可被蛋白酶体抑制剂MG-132阻断。它还能降解在SN-N-SH和NCI H3122细胞中表达的ALK融合蛋白EML4-ALK及含有苯丙氨酸至亮氨酸替换突变(ALKF1174L)的ALK。AP-1对依赖ALK的Karpas-299细胞具有细胞毒性(IC50 = 0.1265 nM),但对非ALK依赖的THP-1细胞无细胞毒性(IC50 = 2,704 nM)。在给药剂量为25, 50, 和100 mg/kg时,能减小NCI H3122小鼠移植瘤模型中的肿瘤体积。 |